| Autor: |
Hartz, R. A., Nanda, K. K., Ingalls, C. L., Ahuja, V. T., Molski, T. F., Zhang, G., Wong, H., Peng, Y., Kelley, M., Lodge, N. J., Zaczek, R., Gilligan, P. J., Trainor, G. L. |
| Zdroj: |
Journal of Medicinal Chemistry; September 2004, Vol. 47 Issue: 19 p4741-4754, 14p |
| Abstrakt: |
A growing body of evidence suggests that CRF1 receptor antagonism offers considerable therapeutic potential in the treatment of diseases resulting from elevated levels of CRF, such as anxiety and depression. A series of novel 1,2,3,7-tetrahydro-6H-purin-6-one and 3,7-dihydro-1H-purine-2,6-dione derivatives was synthesized and evaluated as corticotropin releasing factor-1 (CRF1) receptor antagonists. Compounds within this series, represented by compound 12d (IC50 = 5.4 nM), were found to be highly potent CRF1 receptor antagonists. In addition, compounds 12d and 12j were determined to be selective CRF1 antagonists. The synthesis, structure−activity relationships and pharmacokinetic properties of compounds within this series is presented. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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